M2 L3-L4 Flashcards by CHESKA CIANNELLE FRANCISCO

Q

provide certain functional properties to the drug and dosage forms
affect product performance in vivo

A

EXCIPIENTS

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Q

main purpose is to improve product’s performance
NO therapeutic effect
pharmaceutically INACTIVE

A

EXCIPIENTS

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Q

main purpose is to improve product’s performance
NO therapeutic effect
pharmaceutically INACTIVE

A

EXCIPIENTS

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Q

MOST COMMON excipient
compatible with most of the drugs EXCEPT basic substances

A

LACTOSE

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Q

LACTOSE is NOT compatible with ____ substances

A

BASIC

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Q

an excipient that is the ONLY INORGANIC SALT that is a DILUENT

A

DIBASIC CALCIUM PHOSPHATE

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Q

opaquant in HARD gel capsules

A

TITANIUM DIOXIDE

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Q

FUNCTIONAL PROPERTIES OF EXCIPIENTS

improve the ____ of the active drug

for TABLETS

A

COMPRESSIBILITY

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Q

FUNCTIONAL PROPERTIES OF EXCIPIENTS

____ the drug against degradation

A

STABILIZE

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Q

FUNCTIONAL PROPERTIES OF EXCIPIENTS

____ gastric irritation

A

decrease

through specific salts / coating

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Q

FUNCTIONAL PROPERTIES OF EXCIPIENTS

____ of drug absorption

A

CONTROL THE RATE

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Q

FUNCTIONAL PROPERTIES OF EXCIPIENTS

____ drug bioavailability

A

INCREASE

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Q

EFFECTS of Excipients on DISSOLUTION

promote drug RELEASE
INCREASE dissolution (FASTER)

A

DISINTEGRANT

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Q

EFFECTS of Excipients on DISSOLUTION

REPEL water (decrease wettability of powders)
aid in the manufacturing process
DECREASE (if used in large quantities)
0.25 to 5% w/w is the LIMIT

A

LUBRICANTS

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Q

EFFECTS of Excipients on DISSOLUTION

DISINTEGRANT

A

INCREASE dissolution
FASTER dissolution

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Q

EFFECTS of Excipients on DISSOLUTION

LUBRICANTS

A

DECREASE dissolution (if used in large quantities)

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Q

EFFECTS of Excipients on DISSOLUTION

what is the LIMIT of LUBRICANTS

A

0.25 - 5% w/w

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Q

EFFECTS of Excipients on DISSOLUTION

CROSSLINK upon AGING (formation of chemical bonds)
DECREASE dissolution
TOO MUCH binding = HARDER to dissolve

A

COATING (shellac)

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Q

EFFECTS of Excipients on DISSOLUTION

COATING

A

DECREASE
due to too much binding = harder to dissolve

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Q

EFFECTS of Excipients on DISSOLUTION

DECREASE SURFACE TENSION (low concentration) = INCREASE dissolution
form MICELLES (high concentration) = DECREASE dissolution

A

SURFACTANTS

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Q

EFFECTS of Excipients on DISSOLUTION

SURFACTANTS:
low concentration

A

INCREASE dissolution

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Q

EFFECTS of Excipients on DISSOLUTION

SURFACTANTS:
high concentration

A

DECREASE dissolution

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Q

EFFECTS of Excipients on DISSOLUTION

INCREASE viscosity of the medium due to mechanical hindrance
DECREASE the rate of dissolution because particles cannot move due to high viscosity

A

SUSPENDING AGENT

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Q

EFFECTS of Excipients on DISSOLUTION

SUSPENDING AGENT

A

DECREASE the rate of dissolution

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# **EFFECTS of Excipients on DISSOLUTION** * **CHANGE** the **pH** of the **medium** surrounding the active drug substance * in the case of **Aspirin**, dissolution is **increased** due to the formation of **water soluble complex**

SODIUM BICARBONATE

# **EFFECTS of Excipients on DISSOLUTION** SODIUM BICARBONATE: **Aspirin**

INCREASE dissolution due to formation of water soluble complex

# **EFFECTS of Excipients on DISSOLUTION** * forms an **INSOLUBLE complex** with TETRACYCLINE * **DECREASE** dissolution

CALCIUM CARBONATE

# **EFFECTS of Excipients on DISSOLUTION** CALCIUM CARBONATE: **Tetracycline**

DECREASE dissolution due to the formation of insoluble complex

these are the **MOST COMMON LUBRICANTS**

STEARATES

# **EFFECT of LUBRICANTS on DISSOLUTION and ABSORPTION** what is the effect in drug DISSOLUTION if there is a **LESSER** concentration of Mg stearate

GREATER amount of drg dissolved

# **EFFECT of LUBRICANTS on DISSOLUTION and ABSORPTION** what is the effect on drug ABSORPTION if there is **LESSER** concentration of Mg stearate

BETTER absorption in terms of rate & extent

# **EFFECT of EXCIPIENTS on ABSORPTION** ____ **solubility** ____ rate of **absorption**

INCREASE

# **EFFECT of EXCIPIENTS on ABSORPTION** ____ **retention time** in GIT ____ the amount of drug to be **absorbed**

INCREASE

# **EFFECT of EXCIPIENTS on ABSORPTION** acts as ____ to **increase** drug **DIFFUSION** across intestinal wall

CARRIERS

# **EFFECT of EXCIPIENTS on ABSORPTION** may ____ drug **dissolution** and thus **REDUCE** drug **absorption**

RETARD

* deals with the **manufacturing factors** and **physicochemical properties** influencing the **rate & extent** of drug **absorption** from the site of administration of a drug * these are considered **DURING** manufacturing process

BIOPHARMACEUTICS CONSIDERATIONS

# **BIOPHARMACEUTICS CONSIDERATIONS** are used to **anticipate** ____ arising from **poor absorption** of a candidate drug

potential clinical problems

# **BIOPHARMACEUTICS CONSIDERATIONS** are used to ____ of **newly** developed compounds

optimize bioavailability

# **ESSENTIAL ELEMENTS of the BIPHARMACEUTICAL CONSIDERATIONS** * studies done to decide the ____ of the drug to be used, for example, **salt** and **particle size**

PHYSICOCHEMICAL NATURE | if hydrophilic or lipophilic

# **ESSENTIAL ELEMENTS of the BIPHARMACEUTICAL CONSIDERATIONS** the ____ of these studies in relation to the **preclinical studies** with the drug | BASIC properties should be ESTABLISHED

TIMING

# **ESSENTIAL ELEMENTS of the BIPHARMACEUTICAL CONSIDERATIONS** the **determination** of the ____ and ____ characteristics

SOLUBILTIY and DISSOLUTION

# **ESSENTIAL ELEMENTS of the BIPHARMACEUTICAL CONSIDERATIONS** the **evaluation** of ____ and ____ studies

DRUG ABSORPTION and PHYSIOLOGICAL DISPOSITION

# **ESSENTIAL ELEMENTS of the BIPHARMACEUTICAL CONSIDERATIONS** the **design** and **evalutation** of the ____

FINAL DRUG FORMULATION

the **FINISHED** drug product should **meet** the ____ by delivering the drug with **maximum bioavailability** and **minimum adverse effects**

THERAPEUTIC OBJECTIVE

these are the **desired THERAPEUTIC RESPONSE** and the type of frequency of adverse reactions

PHARMACODYNAMIC CONSIDERATIONS

# **PHARMACODYNAMIC CONSIDERATIONS** * it influences the **TYPE OF FORMULATION** manufactured

THERAPEUTIC OBJECTIVE

# **PHARMACODYNAMIC CONSIDERATIONS** THERAPEUTIC OBJECTIVE: * which form of **Nitroglycerin** allows **quick release** of the drug and uses a **shorter route** to the site of action * this is the **desired response** to **anginal attack**

NITROGLYCERIN SL (sublingual)

treatment for **ANGINA PECTORIS**

NITROGLYCERIN SL

# **PHARMACODYNAMIC CONSIDERATIONS** THERAPEUTIC OBJECTIVE: * this is the form used for **PROPHYLACTIC treatment** for **CHRONIC diseases** because they require **long term use** of the drug, so **once daily dosing** is preferred

EXTENDED or CONTROLLED RELEASE

# **PHARMACODYNAMIC CONSIDERATIONS** * **INHALED** drugs for local action are **efficiently delivered** into the lungs = **reducing** the amount needed to **reach** the **therapeutic effect** = **reducing systemic side effects**

TYPE & FREQUENCY OF TOXIC and/or ADVERSE REACTIONS

# **PATIENT CONSIDERATIONS** this is one of the **important** considerations because it may result from: * poor product attributes, such as **difficulty in swallowing**, **disagreeable odor**, **bitter taste** * **too frequent** and/or **unusual dosage** requirements * pharmacodynamic factors, such as **side effects** of the drug or an **allergic reaction**

PATIENT COMPLIANCE

# **DRUG PRODUCT CONSIDERATIONS** * another important consideration in achieving **therapeutic outcome** * **NEW APPROACHES** are being developed to **deliver** drugs **safely** and **improve efficacy** and **patient complaince**

DRUG DELIVERY

# **DRUG PRODUCT and DELIVERY SYSTEM FORMULATION CONSIDERATIONS** GENERAL CONSIDERATIONS

* appropriate DOSAGE FORM * BIOAVAILABILITY * RATE LIMITING STEP

# **DRUG PRODUCT and DELIVERY SYSTEM FORMULATION CONSIDERATIONS** GENERAL CONSIDERATIONS: this depends on; * **physical** and **chemical properties** of the drug * **dose** of the drug * **route** of administration * type of **drug delivery system** required * desired **therapeutic effect** * **physiologic release** of the drug from the delivery system * **bioavailability** of the drug at the absorption site * **pharmacokinetics** and **pharmacodynamics** of the drug

APPROPRIATE DOSAGE FORM

# **DRUG PRODUCT and DELIVERY SYSTEM FORMULATION CONSIDERATIONS** GENERAL CONSIDERATIONS: * the **MORE complicated** the formulation, the **GREATER** the potential problem * controlled-release, enteric coated, transdermal patch * depends on the **succession of rate processes**; * attrition, disintegration, or deaggregation of the drug product * dissolution * convection and diffusion * absorption

BIOAVAILABILITY

# **DRUG PRODUCT and DELIVERY SYSTEM FORMULATION CONSIDERATIONS** GENERAL CONSIDERATIONS: * NOT ALWAYS the **first step** but ALWAYS the **SLOWEST STEP** if other properties of the drug are considered (formulation etc.)

RATE LIMITING STEP

# **DRUG PRODUCT and DELIVERY SYSTEM FORMULATION CONSIDERATIONS** GENERAL CONSIDERATIONS: * what is the **RATE LIMITING STEP** of **CONVENTIONAL solid drugs (caps, tabs)**

DISSOLUTION | 1st step: disintegration - fast due to disintegrants RLS: dissolution

# **DRUG PRODUCT and DELIVERY SYSTEM FORMULATION CONSIDERATIONS** GENERAL CONSIDERATIONS: * what is the **RATE LIMITING STEP** for **CONTROLLED-** or **SUSTAINED-RELEASE** products

the RELEASE of the drug | release is INTENDED to be SLOW

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** * MOST **BIOVAILABLE** form * **NO dissolution** step is necessary

SOLUTIONS

* these are inteded to be dissolved in the **MOUTH** * **NO SWALLOWING** is required

ORAL

* these are drugs that **SHOULD BE SWALLOWED**

PERORAL

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** these are often used as **reference preaparation** for **solid peroral formulations**

PERORAL SOLUTIONS

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** SOLUTIONS: * has **GOOD BIOAVAILABILITY** since **alcohol** aids in **solubility**

ELIXIR

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** SOLUTIONS: * **VISCOSITY** interferes with **dilution** and **GI contents** * has **ethanol** as preservative

SYRUPS

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** * Bioavailability is **similar** to that of solutions because the finely divided particles are dispersed provide large surface area for rapid dissolution * **HIGHLY viscous** suspensions may **PROLONG** gastric emptying, **SLOW** drug dissolution, and **DECREASE** the absorption rates

SUSPENSIONS

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** SUSPENSIONS: * what is the effect of **HIGHLY viscous** suspensions

PROLONG gastric emptying SLOW drug dissolution DECREASE absorption rates

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** * **COATING** of capsule shell or the drug particles within the capsule affect bioavailability * **HARD** gelatin capsule -- bioavailability is **good** * **SOFT** gelatin capsule -- has **better bioavailability** than compressed tablets (if the drug is NOT in hydrophobic vehicle)

CAPSULES

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** CAPSULES: * bioavalabilty is **GOOD**

HARD GEL CAPS

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** CAPSULES: * has **BETTER bioavailability** than compressed tabs (if the drug is not in hydrphobic vehicle)

SOFT GEL CAPS

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** CAPSULES: * may affect the bioavailability due to **change** in **moisture content**

AGING and STORAGE

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** CAPSULES: * effects if there is **SURFACE ACTIVE VEHICLE**

DISPERSE/EMULSIFIES DRUG RAPID dissolution rate

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** CAPSULES: * effects if there is **NON-SURFACE ACTIVE VEHICLE**

FORMS DRUG-RICH SURFACE LAYER RETARDS/PREVENTS DISSOLUTION

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** * Bioavailability is **affected** by the **excipients**

COMPRESSED TABLETS

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** COMPRESSED TABLETS: * determines the **drug RELEASE**

DISINTEGRANTS

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** COMPRESSED TABLETS: * **HIGH** concentration **reduce** the **wetting** of particles, **SLOWING** drug **dissolution**

LUBRICANTS

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** COMPRESSED TABLETS: * **ENHANCE** drug **dissolution**

SURFACTANTS

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** COMPRESSED TABLETS TYPES: * may affect the **RELEASE RATE** of the drug * the **initial step** is **BREAKING** the coating first followed by disintegration

COATED COMPRESSED TABLET

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** COMPRESSED TABLET TYPES: * **DELAY RELEASE** of the drug * intended to be released **2 hours after administration** since the drug travels from the stomach to the **small intestine** where the coat disrupts

ENTERIC COATING

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** COMPRESSED TABLET TYPES: * **ENETRIC coating** is **pH dependent** and it only breaks at what pH

ALKALINE pH

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** * **DOSE DUMPING** is a problem * CONTROLLED release or SUSTAINED action dosage forms allow **two-fold reduction** in dosing frequency; instead of 2-3 dos per day, it will become **once daily dosing** * produce a **flat**, **sustained plasma concentration** that **avoids toxicity** or **lack of efficacy**

MODIFIEED RELEASE DOSAGE FORMS

* it is the **abrupt**, **uncontrolled release** of a large amount of drug * caused by **improper taking** of drug, **improper formulation**, **crushing/chewing** * could lead to **overdosage**

DOSE DUMPING

DISADVANTAGE of **conventional dosage forms** given at various time interval

there is a FLUCTUATION of plasma concetration

MODIFIED release drug products

* Delayed release (enteric coated) * Extended release (ER) -- Controlled & Sustained * Orally Disintegrating Tablet

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** * are **controlled release devices** that contain the drug for the **systemic absorption** after **topical application** to the **SKIN SURFACE**

TRANSDERMAL DRUG DELIVERY SYSTEM

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** * **drug carrier systems** that place the drug at or near the receptor site * **Protein drug carrier**, **liposomes**, **nanoparticles**, **monoclonal antibodies**

TARGETED DRUG DELIVERY SYSTEM

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** TARGETED DRUG DELIVERY SYSTEM: * this is common to what type of cells

CANCER CELLS

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** TARGETED DRUG DELIVERY SYSTEM: * this is where the **drug** and **targeting molecules** **BINDS**

NANOPARTICLE

# **DRUG PRODUCT and DELVIERY SYSTEM FORMULATION** * used to **control** drug delivery for **localized** or **systemic** drug effects * **INSERTED** into a variety of cavities such as vagina, buccal cavity, and skin * intended to deliver the drug **SLOWLY over long periods of time**

INSERTS, IMPLANTS, AND DEVICES

# **ROUTE OF ADMINISTRATION** * **INSIDE** the blood vessels * **NO absorption** phase

INTRAVASCULAR

# **ROUTE OF ADMINISTRATION** * **OUTSIDE** the blood vessels

EXTRAVASCULAR

# **ROUTE OF ADMINISTRATION** INTRAVASCULAR

Intravenous (bolus, infusion) Intraarterial Intracardiac

# **ROUTE OF ADMINISTRATION** EXTRAVASCULAR: **parenteral**

Intramuscular Subcutaneous Intraarticular Intrathecal

# **ROUTE OF ADMINISTRATION** EXTRAVASCULAR: **Enteral**

Peroral Oral (buccal, sublingual) Rectal

# **IV INTRAVASCULAR** * **RAPID** achievement of concentration * **precise delivery** of dosage * **easy to titrate** dose * **HIGH initial concentration** -- prone to toxicity * **invasive** - high risk of infection * requires a certain **level** of **skill**

INTRAVENOUS INJECTION

# **IV INTRAVASCULAR** INTRAVENOUS INJECTION: * for **BULK doses** * injected **directly** into the bloodstream * acts **rapidly** * **side effects** occur **rapidly** * **100% bioavailability** * rate is considered **INSTANTANEOUS** * **IMMEDIATE** effect * **high risk** of adverse effects * possible **anaphylaxis**

IV BOLUS

# **IV INTRAVASCULAR** INTRAVENOUS INJECTION: * **SLOWLY** administered * given at a **CONSTANT INPUT** rate * constant rate maintains a relative **constant plasma drug concentration** * **100% bioavailability** * **controlled** by infusion rate * drug levels are **MORE PRECISELY CONTROLLED** * **large** fluid volumes may be injected * may use drugs with **POOR LIPID SOLUBILITY** and/or **IRRITATING DRUGS** * **skill** is required * **tissue damage** at the injection site fue to frequent injection

IV INFUSION

# **IV INTRAVASCULAR** * drug is injected into **specific ARTERY** to achieve a high concentration * used for **DIAGNOSTIC AGENTS** and occasionally for **chemotherapy**

IntraARTERIAL injection

# **EXTRAVASCULAR | PARENTERAL ROUTES** * for **SUSTAINED** drug action * **DEPOT** injection: drugs are deposited in **MUSCLES**, then **slowly diffusing** into the blood vessels; drug is **NOT** intended to **act rapidly** * **RAPID** bioavailablity from **aqeuous** solution * **SLOW** absorption fron **non-aqeuous** solution * **EASIER to inject** than IV * **Larger** volume may be used compared to SC injection * **PAINFUL** * absorption rate depends on **muscle group** * the rate of absorption depends on; * vascularity of the muscle site * lipid solubiltiy of the drug * formulation matrix

IntraMUSCULAR injection

# **EXTRAVASCULAR | PARENTERAL ROUTES** * drug absorption is **LESS RAPID** than IM * region is **LESS VASCULAR** than muscle tissues which means **LESS BLOOD VESSELS** that can carry the drug away from the site of administration * drug is injected into the **FATTY/ADIPOSE tissues** * Bioavailability is **PROMPT** form **aqueous** solution * Bioavailability is **SLOW** from **repository** formulations * generally used for **INSULIN** injection * absorption rate depends on **blood flow** and **injection volume**

SUBCUTANEOUS INJECTION

# **EXTRAVASCULAR | PARENTERAL ROUTES** INTRAMUSCULAR: * **absorption rate** depends on ____ and ____

muscle group injected blood flow

# **EXTRAVASCULAR | PARENTERAL ROUTES** INTRAMUSCULAR: * **Bioavailability** -- from **aqueous** solution

RAPID

# **EXTRAVASCULAR | PARENTERAL ROUTES** INTRAMUSCULAR: * **Bioavailability** -- from **non-aqueous** solution

SLOW absoprtion

# **EXTRAVASCULAR | PARENTERAL ROUTES** SUBCUTANEOUS: * **Bioavailability** -- from **aqueous** solution

PROMPT

# **EXTRAVASCULAR | PARENTERAL ROUTES** SUBCUTAENOUS: * **Bioavailability** -- from **repository** formulations | these are formulations that are intended to be released SLOWLY

SLOW

# **EXTRAVASCULAR | PARENTERAL ROUTES** SUBCUTAENOUS: * **absorption rate** depends on ____ and ____

blood flow injection volume

# **EXTRAVASCULAR | PARENTERAL ROUTES** generally used for **INSULIN** injection

SUBCUTANEOUS

# **EXTRAVASCULAR | PARENTERAL ROUTES** MISCELLANEOUS: * into the **JOINT**

Intra-articular

# **EXTRAVASCULAR | PARENTERAL ROUTES** MISCELLANEOUS: * into the **DERMIS**

IntraDERMAL (intracutaneous) injection

# **EXTRAVASCULAR | PARENTERAL ROUTES** MISCELLANEOUS: * into the **SPINAL FLUID**

Intrathecal

# **EXTRAVASCULAR | ENTERAL ADMINISTRATION** * Bioavailability is **RAPID** from **lipid soluble drugs**; provide **QUICK RESPONSE** due to **fast dissolution** and **lesser distance travelled** by the drug * the distance from the mouth to the **vena cava** is **SHORTER** as compared to the drug absorbed from the small intestine * **BY PASS** the liver and any **first-pass effect**; MORE drug gets into the systemic circulation * **NOT** suited for drugs with **high doses**

BUCCAL and SUBLINGUAL

# **EXTRAVASCULAR | ENTERAL ADMINISTRATION** * drug is in contact with the **mucosal surface** of the **CHEEK**

BUCCAL

# **EXTRAVASCULAR | ENTERAL ADMINISTRATION** * placed **UNDER the TOUNGE**

SUBLINGUAL

# **EXTRAVASCULAR | ENTERAL ADMINISTRATION** * the drug is **SWALLOWED** and **undergoes absorption** from the GIT through the **mesenteric circulation** to the **hepatic protal vein** * **MOST CONVINIENT** * **SAFEST** route * may use **limited-release** and **controlled-release** drug products * drugs may **NOT** be absorbed from the GIT **consistently** or **completely** * the drug may be **digested** by GI enzyzmes or **decomposed** by the **acid pH** of the stomach * the drug may **irritate** epithelial cells or complex with the content of the GIT * some drugs may be **incompletely absorbed** because of **first-pass effect** or **pre-systemic circulation** * the absorption rate may be **erratic** because of **elayed gastric emptying** or **changes in intestinal motility**

ORAL or PERORAL

# **EXTRAVASCULAR | ENTERAL ADMINISTRATION** ORAL or PERORAL: * this is the **primary ABSORPTION site**

DUODENAL REGION

# **EXTRAVASCULAR | ENTERAL ADMINISTRATION** ORAL or PERORAL: * affects **arrival** of the drug in the **duodenum**

altered gastric emptying

# **EXTRAVASCULAR | ENTERAL ADMINISTRATION** ORAL or PERORAL: * affects the **contact time** with the **epithelial cells**

PERISTALTIC MOVEMENT

# **EXTRAVASCULAR | ENTERAL ADMINISTRATION** * absorption occurs upon **diffusion** of drugs across the **mucosal surface** of the **RECTUM** * **by pass** the liver and **first-pass effect** BUT **PARTIAL only** * absorption may be **erratic** * patient **discomfort**

RECTAL

# **EXTRAVASCULAR | ENTERAL ADMINISTRATION** RECTAL: * region of the rectum that is connected to the **inferior hemorrhoidal vein**

INFERIOR

# **EXTRAVASCULAR | ENTERAL ADMINISTRATION** RECTAL: * region of the rectum that is connected to the **hepatic portal vein**

SUPERIOR

# **EXTRAVASCULAR | ENTERAL ADMINISTRATION** RECTAL: * in which regions can a drug **by pass** the **first-pass effect**

middle-inferior

# **RESPIRATROY TRACT ADMINISTRATION** * drugs in **solution** or **suspension** is administered either as **spray** or **drops** * used for **local** or **systemic effect**

INTRANASAL

# **RESPIRATROY TRACT ADMINISTRATION** INTRANASAL: * has **better bioavailability** when given intranasal

LORAZEPAM

# **RESPIRATROY TRACT ADMINISTRATION** INTRANASAL: * **intranasal administration is BETTER** than IM injection in terms od the concentration available systemically * can cause **anterograde amnesia**

MIDAZOLAM

# **RESPIRATROY TRACT ADMINISTRATION** INTRANASAL: * **intranasal** and **IV administration** are **almost comparable** in terms of bioavailability

MORPHINE

# **RESPIRATROY TRACT ADMINISTRATION** * drugs are administered **into the respiratory system** by **ORAL INHALATION** * for **local** and/or **systemic effects** * drugs are formulated as **AEROSOLS** or **inhalation solutions** * **RAPID** absorption and **RAPID** onset of activity * **AVOIDANCE** of first pass effects or metabolism * **LOCALIZATION** of drug activity to the lungs and **MINIMUM** systemic toxicity

PULMONARY INHALATION

# **RESPIRATROY TRACT ADMINISTRATION** PULMONARY INHALATION: * these exhibits RAPID **absorption** and RAPID **onset of activity**

BRONCHODILATORS | B2 agonists

# **RESPIRATROY TRACT ADMINISTRATION** PULMONARY INHALATION: * drugs that can AVOID **first pass effects** or **metabolism**

ISOPROTERENOL BITOLTEROL

# **RESPIRATROY TRACT ADMINISTRATION** PULMONARY INHALATION: * these drugs exhibit **localization** of drug activity to the lungs and **minimum** systemic toxicity

Corticosteroid - safer when inhaled Dexamethasone

# **RESPIRATROY TRACT ADMINISTRATION** PULMONARY INHALATION: * **better absorption** when administered through **nasal route**

MIDAZOLAM

# **TRANSDERMAL and TOPICAL ADMINISTRATION** * placement of drug on the **SKIN SURFACE** for **systemic absorption** * drugs should be **POTENT** at **LOW DOSES**

TRANSDERMAL (Percutaneous)

# **TRANSDERMAL and TOPICAL ADMINISTRATION** TRANSDERMAL (Percutaneous): * drugs

Nicotine Nitroglycerin Scopolamine Clonidine

# **TRANSDERMAL and TOPICAL ADMINISTRATION** TRANSDERMAL (Percutaneous): * the **VERY FIRST** transdermal drug

SCOPOLAMINE

# **TRANSDERMAL and TOPICAL ADMINISTRATION** * drugs are applied for **LOCAL** effect only * **antibacterials** * **local anesthetics**

TOPICAL

# **TRANSDERMAL and TOPICAL ADMINISTRATION** what is the ADVANTAGE of **transdermal** over oral

the drug plasma concentration is STEADY (non-fluctuating)

# **TRANSDERMAL and TOPICAL ADMINISTRATION** FACTORS THAT INFLUENCE PERCUTANEOUS ABSORPTION

* Site of application * Condition of skin * Hydration of skin * Temperature * Vehicle

# **TRANSDERMAL and TOPICAL ADMINISTRATION** * also known as **PERMEATION ENHANCERS** * incorporated to drug product to **promote systemic drug absorption** from the application site * an excipient or physical approaches

ABSORPTION ENHANCERS

# **TRANSDERMAL and TOPICAL ADMINISTRATION** ABSORPTION ENHANCERS: * promotes the delivery of **ESTROGEN** (Estraderm - Estradiol Transdermal system) through the **stratum corneum** of the skin

ETHANOL

# **TRANSDERMAL and TOPICAL ADMINISTRATION** ABSORPTION ENHANCERS: * used to **enhance percutaneous absorption** of **HYDROCORTISONE ointment**

ULTRASOUND (phonophoresis or sonophoresis)

# **TRANSDERMAL and TOPICAL ADMINISTRATION** ABSORPTION ENHANCERS: * other terms for **Ultrasound**

phonophoresis sonophoresis

# **MISCELLANEOUS ROUTES** * generally used for **LOCAL** therapeutic activity

ophthalmic otic urethral vaginal